Benzothiazinones: a novel class of adenosine receptor antagonists structurally unrelated to xanthine and adenine derivatives.

@article{Gtschow2012BenzothiazinonesAN,
  title={Benzothiazinones: a novel class of adenosine receptor antagonists structurally unrelated to xanthine and adenine derivatives.},
  author={Michael G{\"u}tschow and Miriam Schlenk and J{\"u}rgen G{\"a}b and Minka Paskaleva and Mohamad Wessam Alnouri and Silvia Scolari and Jamshed Iqbal and Christa E. M{\"u}ller},
  journal={Journal of medicinal chemistry},
  year={2012},
  volume={55 7},
  pages={3331-41}
}
2-(Acyl)amino-4H-3,1-benzothiazin-4-ones and related thienothiazinones were identified as structurally novel antagonists at adenosine receptors (ARs). 6-Methyl-2-benzoylamino-4H-3,1-benzothiazin-4-one (10d) was found to be a balanced AR antagonist with affinity for all human (h) subtypes (K(i) hA(1) 65.6 nM; hA(2A) 120 nM; hA(2B) 360 nM; hA(3) 30.4 nM), while in rat (r), 10d was a highly potent A(1)-selective antagonist (rA(1) 7.7 nM; rA(2A) 546 nM; rA(2B) 679 nM, rA(3) >10000 nM). 2-(4… CONTINUE READING

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benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A2B adenosine receptor antagonists

  • S. Weyler, F. Fülle, +4 authors C. E. Müller
  • J. Med. Chem
  • 2012

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